Development and validation of a fluorescence technology for both primary and secondary screening of kinases that facilitates compound selectivity and site-specific inhibitor determination

Assay and Drug Development Technologies

Volumn 2, Issue 2, 2004, Pages 171-181

  Morgan, Aric G ^a   McCauley, Timothy J ^a   Stanaitis, Michael L ^a   Mathrubutham, Mahesh ^a   Millis, Sherri Z ^a  

^a Pierce Biotechnology ^*  (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 [N,O BIS(5 ISOQUINOLINESULFONYL) N METHYLTYROSYL] 4 PHENYLPIPERAZINE; 2 (2 AMINO 3 METHOXYPHENYL)CHROMONE; 2 MORPHOLINO 8 PHENYLCHROMONE; 2 [1 (3 AMIDINOTHIOPROPYL) 1H INDOL 3 YL] 3 (1 METHYL 1H INDOL 3 YL)MALEIMIDE; 4 (4 FLUOROPHENYL) 2 (4 HYDROXYPHENYL) 5 (4 PYRIDYL)IMIDAZOLE; 4 (4 FLUOROPHENYL) 2 (4 METHYLSULFINYLPHENYL) 5 (4 PYRIDYL)IMIDAZOLE; ADENOSINE TRIPHOSPHATE; AMINO ACID; CHROMOGENIC SUBSTRATE; DETERGENT; N [2 (4 BROMOCINNAMYLAMINO)ETHYL] 5 ISOQUINOLINESULFONAMIDE; ORGANIC COMPOUND; PHOSPHATASE; PHOSPHOPROTEIN; PHOSPHOTRANSFERASE; PHOSPHOTRANSFERASE INHIBITOR; RADIOACTIVE MATERIAL; WORTMANNIN;

AMINO ACID SEQUENCE; ARTICLE; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; DRUG DETERMINATION; DRUG SCREENING; DRUG SELECTIVITY; ENZYME ACTIVITY; ENZYME ASSAY; ENZYME INHIBITION; ENZYME SUBSTRATE; FLUORESCENCE ANALYSIS; HIGH THROUGHPUT SCREENING; IC 50; PROTEIN BINDING; PROTEIN PHOSPHORYLATION; SPECTROPHOTOMETRY;

EID: 2442530408     PISSN: 1540658X     EISSN: None     Source Type: Journal    
DOI: 10.1089/154065804323056512     Document Type: Article

References (29)

1. Cohen P: The origins of protein phosphorylation. Nat Cell Biol 2002;4:E127-E130.
2. Blume-Jensen P, Hunter T: Oncogenic kinase signaling. Nature 2001;411:355-365.
3. Nick JA, Young SK, Brown KK, Avdi NJ, Arndt PG, Suratt BT, Janes MS, Henson PM, Worthen GS: Role of p38 mitogen-activated protein kinase in a murine model of pulmonary inflammation. J Immunol 2000;164:2151-2159.
4. Ways DK, Sheetz MJ: The role of protein kinase C in the development of the complications of diabetes. Vitam Horm 2000;60:149-193.
5. Vlahos CJ, McDowell SA, Clerk A: Kinases as therapeutic targets for heart failure. Nat Rev Drug Discov 2003;2: 99-113.
6. Cohen P: The development and therapeutic potential of protein kinase inhibitors. Curr Opin Chem Biol 1999;3:459-465.
7. High-Throughput Screening 2002: New Strategies and Technologies. HighTech Business Decisions, Moraga, CA, 2002.
8. Muller MO, Meylan-Bettex M, Eckstein F, Martinoia E, Siegenthaler PA, Bovet L: Lipid phosphorylation in chloroplast envelopes. Evidence for galactolipid CTP-dependent kinase activities. J Biol Chem 2000;275:19475-19481.
9. Versteeg HH, Nijhuis E, van den Brink GR, Evertzen M, Pynaert GN, van Deventer SJ, Coffer PJ, Peppelenbosch MP: A new phosphospecific cell-based ELISA for p42/p44 mitogen-activated protein kinase (MAPK), p38 MAPK, protein kinase B and cAMP-response-element-binding protein. Biochem J 2000;350:717-722.
10. Sills MA, Weiss D, Pham Q, Schweitzer R, Wu X, Wu JJ: Comparison of assay technologies for a tyrosine kinase assay generates different results in high throughput screening. J Biomol Screen 2002;7:191-214.
11. Wu JJ, Yarwood DR, Pham Q, Sills MA: Identification of a high-affinity anti-phosphoserine antibody for the development of a homogeneous fluorescence polarization assay of protein kinase C. J Biomol Screen 2000;5:23-30.
12. Amir-Zaltsman Y, Mazor O, Gayer B, Scherz A, Salomon Y, Kohen F: Inhibitors of protein tyrosine phosphorylation: preliminary assessment of activity by time-resolved fluorescence. Luminescence 2000;15:377-380.
13. Yeh RH, Yan X, Cammer M, Bresnick AR, Lawrence DS: Real time visualization of protein kinase activity in living cells. J Biol Chem 2002;277:11527-11532.
14. Fowler A, Swift D, Longman E, Acornley A, Hemsley P, Murray D, Unitt J, Dale I, Sullivan E, Coldwell M: An evaluation of fluorescence polarization and lifetime discriminated polarization for high throughput screening of serine/threonine kinases. Anal Biochem 2002;308:223-231.
15. Comley J: Assay interference - a limiting factor in HTS? Drug Discov World 2003;4:91-98.
16. Turek TC, Small EC, Bryant RW, Hill WA: Development and validation of a competitive AKT serine/threonine kinase fluorescence polarization assay using a product-specific anti-phospho-serine antibody. Anal Biochem 2001; 299:45-53.
17. Sorensen ES, Petersen TE: Identification of two phosphorylation motifs in bovine osteopontin. Biochem Biophys Res Commun 1994;198:200-205.
18. Sun T, Campbell M, Gordon W, Arlinghaus RB: Preparation and application of antibodies to phosphoamino acid sequences. Biopolymers 2001;60:61-75.
19. Hawkins J, Zheng S, Frantz B, LoGrasso P: p38 map kinase substrate specificity differs greatly for protein and peptide substrates. Arch Biochem Biophys 2000;382:310-313.
20. Biondi RM, Cheung PC, Casamayor A, Deak M, Currie RA, Alessi DR: Identification of a pocket in the PDK1 kinase domain that interacts with PIF and the C-terminal residues of PKA. EMBO J 2000;19:979-988.
21. Kojima K, Kitada S, Ogishima T, Ito A: A proposed common structure of substrates bound to mitochondrial processing peptidase. J Biol Chem 2001;276:2115-2121.
22. Neininger A, Thielemann H, Gaestel M: FRET-based detection of different conformations of MK2. EMBO Rep 2001;2:703-708.
23. Turek-Etienne TC, Kober TP, Stafford JM, Bryant RW: Development of a fluorescence polarization AKT serine/threonine kinase assay using an immobilized metal ion affinity-based technology. Assay Drug Dev Technol 2003; 1:545-553.
24. Muszynska G, Dobrowolska G, Medin A, Ekman P, Porath JO: Model studies on iron(III) ion affinity chromatography. II. Interaction of immobilized iron(III) ions with phosphorylated amino acids, peptides and proteins. J Chromatogr 1992;604:19-28.
25. Zhang J-H, Chung T, Oldenburg K: A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 1999;4:67-73.
26. www.Piercenet.com/drugdiscovery.
27. Davies SP, Reddy H, Caivano M, Cohen P: Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J 2000;351:95-105.
28. Knighton DR, Zheng JH, Ten Eyck LF, Xuong NH, Taylor SS, Sowadski JM: Structure of a peptide inhibitor bound to the catalytic subunit of cyclic adenosine monophosphate-dependent protein kinase. Science 1991;253: 414-420.
29. McCauley TJ, Stanaitis ML, Savage MD, Onken J, Millis SZ: IQ technology: development of a universal, homogeneous method for high-throughput screening of kinase and phosphatase activity. JALA 2003;8:36-40.